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HRID 15087作成日:2026年10月24日

Triethylamine → Raf265

https://huagongshe.com/ja/reaction/15087

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物4-(Trifluoromethyl)phenyl isothiocyanateHCID 137134—
反応物2-Chloro-1-methylpyridinium iodideHCID 167069—
反応物1,2-Benzenediamine,n1-methyl-4-[[2-[5-(trifluoromethyl)-1h-imidazol-2-yl]-4-pyridinyl]oxy]-HCID 57531890—
溶媒WaterHCID 962—
溶媒AcetonitrileHCID 6342—
生成物Raf265HCID 1165651861.1%

反応手順

4-Trifluoromethylphenyl isothiocyanate (200 mg, 1 mmol) was added to a mixture of 4-(2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yloxy)-N1-methylbenzene-1,2-diamine (350 mg, 1 mmol) in 3 mL of acetonitrile. After stirring for 20 min at ambient temperature, HPLC analysis showed complete conversion. Triethylamine (0.3 mL, 2.2 mmol) was added followed by 2-chloro-1-methylpyridinium iodide (270 mg, 1.05 mmol). The reaction mixture was heated to 50° C. for 5 h. The heating was stopped and 1.5 mL of water was added. After stirring the mixture for 2 h, the solid was collected by filtration and washed with 2:1 acetonitrile/water (3×1 mL) to afford 317 mg (61%) of the title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07732465B2
出典データセットuspto-grants-2010_06
ORD IDord-41569efb36284549a33e200ea2966f74
出典メモuspto-grants-2010_06